Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
1618 Results for "
Covalent
" in MedChemExpress (MCE) Product Catalog:
Products (1618)
1618 Results for "Covalent" in MCE Product Catalog:
Cat. No.: HY-L024
931 compounds
A histone modification, a covalent post-translational modification (PTM) to histone proteins, includes methylation, phosphorylation, acetylation, ubiquitylation, and sumoylation, etc. In general, histone modifications are catalyzed by specific enzymes that act predominantly at the histone N-terminal tails involving amino acids such as lysine or arginine, as well as serine, threonine, tyrosine, etc. The PTMs made to histones can impact gene expression by altering chromatin structure or recruiting histone modifiers. Histone modifications act in diverse biological processes such as transcriptional activation/inactivation, chromosome packaging, and DNA damage/repair. Deregulation of histone modification contributes to many diseases, including cancer and autoimmune diseases.
MCE owns a unique collection of 931 bioactive compounds targeting Epigenetic Reader Domain, HDAC, Histone Acetyltransferase, Histone Demethylase, Histone Methyltransferase, Sirtuin, etc. Histone Modification Research Compound Library is a useful tool for histone modification research and drug screening.
Cat. No.: HY-112624E
CAS No.: 9004-54-0
Synonyms: Dextran 0.8; Dextran D0.8; Dextran T0.8(MW 640-960)
Cat. No.: HY-112624J
CAS No.: 9004-54-0
Synonyms: Dextran 4; Dextran D4; Dextran T4(MW 3200-4800)
Cat. No.: HY-121501
CAS No.: 121024-51-9
Target:
Research Areas:
Tyrostatin is a peptide inhibitor isolated from Kitasatospora sp. 55. It has a Ki value of 6 nM against serine carboxyl protease (PSCP) from Pseudomonas sp. 101, a Ki value of 2.1 nM against carboxyl protease (XSCP) from Xanthomonas sp. T-22, and a Ki value of 2.6 nM against carboxyl protease (PCP) from Pseudomonas sp. 101. Tyrostatin forms a reversible covalent hemiacetal bond with Ser287 at the active site of PSCP, where Tyr at the P1 position and Leu at the P2 position occupy the S1-S4 subsites of the enzyme. Tyrostatin inhibits the activity of XSCP, specifically blocks the autocatalytic maturation process of PCP precursor under acidic conditions, and also inhibits the protease activity of mature and recombinant PCP in a dose-dependent manner. Tyrostatin does not inhibit KSCP or alcohol-resistant protease J-4, and can serve as a tool for identifying the catalytic residues of PCP .
Cat. No.: HY-124084
CAS No.: 1673556-40-5
Target:
Research Areas:
SW203668 is an irreversible stearoyl CoA desaturase (SCD) inhibitor with an IC50 of 54 nM. SW203668 covalently binds and inhibits SCD, depletes unsaturated fatty acids, and triggers cell death in sensitive cells. SW203668 requires demethylation by CYP4F11 to form its active SCD-inhibiting form; differential CYP4F11 expression drives selective cytotoxicity. SW203668 exerts cytotoxicity toward CYP4F11-expressing non-small cell lung cancer (NSCLC) cells and spares CYP4F11-lacking NSCLC cells. SW203668 inhibits tumor growth in immunodeficient mice bearing CYP4F11-expressing NSCLC xenografts and spares mouse skin sebocytes. SW203668 can be used for the research of non-small cell lung cancer .
Cat. No.: HY-138794A
CAS No.: 2417089-73-5
Target:
Research Areas:
(Rac)-XL177A is the racemic isomer of XL177A (HY-138794). XL177A is a covalent USP7 inhibitor that blocks the deubiquitinase activity of USP7. XL177A destabilizes non-canonical PRC1 complexes or KDM6A and reduces chromatin deposition of H2AK119Ub, thereby relieving the repression of neuronal differentiation programs. Meanwhile, XL177A also regulates the ELOF1-UVSSA-USP7-nuclear β-catenin axis, decreasing the transcription levels of related proteins and the accumulation of nuclear β-catenin. XL177A exerts antiviral effects by reducing the expression levels of coronavirus receptors, and exhibits inhibitory activity against APC-mutated colorectal cancer cells, neuroblastoma, and coronaviruses including SARS-CoV-2 variants. XL177A is mainly used in studies related to colorectal cancer, neuroblastoma, and coronavirus infections .
Cat. No.: HY-149359
CAS No.: 3049485-80-2
Target:
Research Areas:
IHMT-IDH1-053 (compound 16) is a highly selectivity and irreversible IDH1-mutant inhibitor with an IC50 of 4.7 nM for IDH1 R132H. IHMT-IDH1-053 displays high selectivity against IDH1 mutants over IDH1 wt and IDH2 wt/mutants. IHMT-IDH1-053 inhibits 2-hydroxyglutarate (2-HG) production in IDH1 R132H mutant transfected 293T cells (IC50=28 nM). IHMT-IDH1-053 binds to the IDH1 R132H protein in the allosteric pocket adjacent to the NAPDH binding pocket through a covalent bond with residue Cys269. IHMT-IDH1-053 inhibits the proliferation of HT1080 cell line and primary AML cells which both bear IDH1 R132 mutants .
Cat. No.: HY-151833
CAS No.: 2639395-39-2
Target:
Research Areas:
Methyltetrazine-amido-N-bis(PEG4-acid) is a click chemistry reagent containing an azide group. Methyltetrazine-amido-N-bis(PEG4-acid) is a PEG derivative that contains a methyltetrazine group and two acid groups. This reagent can react with TCO-containing compounds to form a stable covalent bond without the catalysis of Cu or elevated temperatures. The inverse-electron demand Diels-Alder cycloaddition reaction of TCO with tetrazines is the fastest bioorthogonal reaction with exceptional selectivity. The terminal carboxylic acid can react with primary amine groups in the presence of activators (e.g. EDC, or HATU) to form a stable amide bond. PEG linker increases the water solubility of the compound. Reagent grade, for research use only . Methyltetrazine-amido-N-bis(PEG4-acid) is a click chemistry reagent, it contains a Tetrazine group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing TCO groups.
Cat. No.: HY-182044
MRTX849-amide-C4-(o)-carborane is a KRAS G12C inhibitor with mutation selectivity for cells expressing KRAS G12C. MRTX849-amide-C4-(o)-carborane shows low intrinsic cytotoxicity in cancer cells. MRTX849-amide-C4-(o)-carborane covalently binds to Cys12 of KRAS G12C, recruits Hsp70, promotes ubiquitination, and induces proteasome-dependent degradation of the target protein. MRTX849-amide-C4-(o)-carborane inhibits the activity of the downstream ERK signaling pathway and induces apoptosis signaling in cancer cells. MRTX849-amide-C4-(o)-carborane is applicable for the research of KRAS G12C-positive cancers .
Cat. No.: HY-184600
Reactive oxygen species responsive hydrogels are a novel class of smart hydrogels, formed by the cross-linking of ROS-responsive modules through covalent, coordination, or supramolecular interactions. Due to the introduction of these ROS-responsive modules, these hydrogels exhibit a sensitive response to the oxidative stress microenvironment present in organisms. PVA-TSPBA hydrogel is a hydrogel formed by the cross-linking polymerization of polyvinyl alcohol (PVA) and the reactive oxygen species-sensitive cross-linking agent N1-(4-benzyl borate)-N3-(4-phenyl borate)N1,N1,N3,N3-tetramethyl-1,3-propanediamine (TSPBA). This hydrogel consists of two parts: a boric acid precursor (TSPBA) and an aqueous solution of PVA. The boric acid bonds on TSPBA and the hydroxyl groups on PVA rapidly cross-link to form borate ester bonds, thus forming the hydrogel.
Cat. No.: HY-189662
Target:
Research Areas:
Y-U0-S is a potent inhibitor of the coronavirus main protease (M pro) and host cathepsins. The IC50 values of Y-U0-S against SARS-CoV-2 M pro, SARS-CoV Mpro, Cathepsin B, and Cathepsin L are 0.81, 1.14, 0.86, and 21.13 μM, respectively. Y-U0-S exhibits broad-spectrum anti-coronavirus activity, with an EC50 of 0.22 μM against wild-type SARS-CoV-2. Y-U0-S forms an irreversible covalent bond with the catalytic site C145 of M pro through its aldehyde warhead, and by optimizing multi-site occupancy of the scaffold to engage conserved residues, it effectively blocks enzyme activity and inhibits viral replication. Y-U0-S can be used for research on COVID-19 .
Cat. No.: HY-D1850
Cat. No.: HY-D3072
Research Areas:
P6-Aggrate is a fluorescent probe for aggregated proteome detection. P6-Aggrate specifically recognizes amorphous aggregated proteomes through non-covalent reversible binding, and its fluorescence enhances after heat-induced protein aggregation. P6-Aggrate reflects the polarity and compactness heterogeneity within aggregated proteomes via emission wavelength shift: short-wavelength emission (blue shift) corresponds to large aggregates with high compactness, while long-wavelength emission (red shift) corresponds to small spots with low compactness (Ex/Em = 488/520-580 nm). P6-Aggrate enables reversible monitoring of the dynamic processes of formation and clearance of stress-induced proteome aggregation such as that induced by MG132 (HY-13259) in living cells. P6-Aggrate can be used in studies related to protein homeostasis imbalance, neurodegenerative diseases and protein aggregation .
Cat. No.: HY-P1348
CAS No.: 1197810-60-8
Synonyms: [Gly8,36,Glu22]-GLP-1 (7-37)
Target:
Research Areas:
Cat. No.: HY-W043748
CAS No.: 38862-24-7
Synonyms: N-Succinimidyl acrylate
Target:
Research Areas:
2,5-Dioxopyrrolidin-1-yl acrylate (N-Succinimidyl acrylate) is a lysine residue modifier and coupling monomer. 2,5-Dioxopyrrolidin-1-yl acrylate covalently modifies the primary amines of lysine residues on monoclonal anti-horseradish peroxidase IgG antibodies, neutralizes positive charges and replaces them with low-affinity acrylate groups. 2,5-Dioxopyrrolidin-1-yl acrylate inhibits the formation of rapid hard coronas on citrate-coated gold nanoparticles, induces antibody unfolding and loss of antigen-binding function, but does not affect the antigen-binding function of antibodies in free solution. 2,5-Dioxopyrrolidin-1-yl acrylate reacts with the ε-amino groups on lysine residues of L-asparaginase, introduces vinyl groups and generates N-hydroxysuccinimide. 2,5-Dioxopyrrolidin-1-yl acrylate regulates the activity of L-asparaginase .
Cat. No.: HY-W089800
CAS No.: 18829-56-6
Synonyms: trans-2-Nonen-1-al
Target:
Research Areas:
trans-2-Nonenal (trans-2-Nonen-1-al) is an endogenous peroxidation product of polyunsaturated fatty acids, acting as an inhibitor of COX and 12-LOX, as well as an inducer of apoptosis. trans-2-Nonenal is also a malodorous compound secreted by the human body, and its content gradually increases with aging. trans-2-Nonenal inhibits the activities of multiple enzymes such as platelet membrane-bound PTPase, preferentially covalently modifies proteins at lysine residues to form immunogenic adducts, and regulates platelet Arachidonic acid (HY-109590) metabolism. trans-2-Nonenal also exhibits significant cytotoxicity, reduces the viability of keratinocytes, promotes their apoptosis, and effectively decreases the thickness of epidermal models and the number of proliferating cells. trans-2-Nonenal is commonly used in studies of thrombotic, atherosclerotic diseases, renal adenocarcinoma, etc. .
Cat. No.: HY-124084A
CAS No.: 2117405-48-6
Target:
Research Areas:
SW203668 TFA is an irreversible stearoyl CoA desaturase (SCD) inhibitor with an IC50 of 54 nM. SW203668 TFA covalently binds and inhibits SCD, depletes unsaturated fatty acids, and triggers cell death in sensitive cells. SW203668 TFA requires demethylation by CYP4F11 to form its active SCD-inhibiting form; differential CYP4F11 expression drives selective cytotoxicity. SW203668 TFA exerts cytotoxicity toward CYP4F11-expressing non-small cell lung cancer (NSCLC) cells and spares CYP4F11-lacking NSCLC cells. SW203668 TFA inhibits tumor growth in immunodeficient mice bearing CYP4F11-expressing NSCLC xenografts and spares mouse skin sebocytes. SW203668 TFA can be used for the research of non-small cell lung cancer .
Cat. No.: HY-163144
CAS No.: 3044084-97-8
DAS-5-oCRBN is a PROTAC molecule with both c‑Src kinase inhibitory activity and target protein degradation activity, with an EC50 of 45 nM for c‑Src binding. DAS-5-oCRBN binds non-covalently to Cereblon and mediates target protein degradation via the ubiquitin-proteasome pathway. DAS-5-oCRBN can catalytically deplete intracellular c‑Src protein, while blocking both the kinase catalytic function of c‑Src and the non-catalytic protein interactions mediated by its SH2 and SH3 domains. DAS-5-oCRBN inhibits tumor cell proliferation and exerts significant anti-proliferative effects on both c‑Src kinase activity-dependent MDA-MB-231 cells and c‑Src protein level-dependent CAL51 cells. DAS-5-oCRBN can be used in cancer-related research such as studies on triple-negative breast cancer and chronic myeloid leukemia .
Cat. No.: HY-179612
Target:
Research Areas:
SARS-CoV-2 3CLpro-IN-34 (Compound 55) is a highly efficient non-covalent inhibitor of the SARS-CoV-2 3CL pro protease (b. SARS-CoV-2 3CL pro protease) with an IC50 of 1.9 μM. SARS-CoV-2 3CLpro-IN-34 can inhibit the 3CL pro protein of SARS-CoV-1, with its IC50 being 3.2 μM, and it shows high selectivity towards host cysteine proteases (such as cathepsins L/K and calpain). SARS-CoV-2 3CLpro-IN-34 exhibits antiviral activity in cells infected with SARS-CoV-2, with its EC50 being 25 μM, and it is not affected by P-gp inhibitors and shows no significant cytotoxicity. SARS-CoV-2 3CLpro-IN-34 can be used for research on SARS-CoV-2 infection .
Cat. No.: HY-181420
CAS No.: 3029184-80-0
Target:
Research Areas:
(S,R,S)-BBO-11818 is an orally active, highly selective (relative to NRAS and HRAS), non-covalent pan-KRAS inhibitor (IC50=28-120 nM). (S,R,S)-BBO-11818 specifically binds to the Switch-II/Helix 3 pocket, disrupts the KRAS:RAF1 interaction by inducing conformational changes, and blocks the MAPK signaling pathway. (S,R,S)-BBO-11818 exhibits significant anti-tumor activity, which not only inhibits cell proliferation and induces apoptosis, but also drives tumor regression in xenograft models. (S,R,S)-BBO-11818 produces synergistic effects when combined with Cetuximab (HY-P9905), anti-PD-1 antibody or PI3Kα inhibitor. (S,R,S)-BBO-11818 is used in the research of KRAS mutation-related malignancies such as pancreatic cancer, non-small cell lung cancer and colorectal cancer .
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
